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Tacrolimus prolonged-release formulation
Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by blocking the phosphatase calcineurin, thereby preventing immune rejection.
Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by blocking the phosphatase calcineurin, thereby preventing immune rejection. Used for Prophylaxis of organ rejection in allogeneic kidney, heart, and liver transplant recipients, Autoimmune diseases including atopic dermatitis and other inflammatory conditions.
At a glance
| Generic name | Tacrolimus prolonged-release formulation |
|---|---|
| Also known as | Advagraf, FK506 |
| Sponsor | Astellas Pharma China, Inc. |
| Drug class | Calcineurin inhibitor |
| Target | Calcineurin (protein phosphatase 2B) |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
Mechanism of action
Tacrolimus binds to the immunophilin FKBP12 and forms a complex that inhibits calcineurin phosphatase activity. This prevents dephosphorylation and nuclear translocation of NFAT (nuclear factor of activated T cells), blocking the transcription of pro-inflammatory cytokines such as IL-2, IL-4, and TNF-α. The prolonged-release formulation provides sustained drug exposure with potentially improved tolerability and reduced dosing frequency compared to immediate-release formulations.
Approved indications
- Prophylaxis of organ rejection in allogeneic kidney, heart, and liver transplant recipients
- Autoimmune diseases including atopic dermatitis and other inflammatory conditions
Common side effects
- Nephrotoxicity / renal impairment
- Hypertension
- Hyperglycemia / new-onset diabetes
- Tremor
- Headache
- Infections
- Hyperkalemia
Key clinical trials
- Clinical Outcome of Delayed or Standard Prograf Together With Induction Therapy Followed by Conversion to Advagraf in Donation After Cardiac (or Circulatory) Death (DCD) Kidney Transplant Recipients (PHASE4)
- A Study of Patient Adherence and Convenience to Immunosuppressive Agents in Newly Liver Transplant (PHASE4)
- Multicentre, Open Label, Randomized, Two-arm, Parallel-group Study to Assess Efficacy and Safety of ENVARSUS® Compared With Tacrolimus Used as Per Current Clinical Practice in the Initial Maintenance Setting in de Novo Kidney Transplant Patients (PHASE4)
- Practical Use of Advagraf de Novo After Kidney Transplantation According to Recipient Genetic Polymorphism (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
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